WHI-P154

Names

[ Name ]:
WHI-P154

[Synonym ]:
2-Bromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol
Phenol, 2-bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-
WHI-P154
jak3 inhibitor ii
2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol

Biological Activity

[Description]:

WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.

[Related Catalog]:

Research Areas >> Cancer

[Target]

EGFR:4 nM (IC50)

JAK3:1.8 μM (IC50)

[In Vitro]

WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively[1]. WHI-P154 significantly enhances the sensitivity of ABCG2-overexpressing cells to its substrates. WHI-P154 (4 μM) moderately sensitizes ABCB1-overexpressing KB-C2 cells to its substrates whereas shows no sensitizing effect on ABCC1-, ABCC2 or ABCC10-mediated drug resistance. Moreover, WHI-P154 (4 μM) causes a significant increase in the intracellular accumulation of [3H]-mitoxantrone in ABCG2-overexpressing cells. WHI-P154 alters the expression levels rather than the localization of the ABCG2 protein in ABCG2-overexpressing cells[2].

[References]

[1]. Changelian PS, et al. The specificity of JAK3 kinase inhibitors. Blood. 2008 Feb 15;111(4):2155-7. Epub 2007 Dec 19.

[2]. Zhang H, et al. WHI-P154 enhances the chemotherapeutic effect of anticancer agents in ABCG2-overexpressing cells. Cancer Sci. 2014 Aug;105(8):1071-8.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
470.3±45.0 °C at 760 mmHg

[ Melting Point ]:
230 °C

[ Molecular Formula ]:
C₁₆H₁₄BrN₃O₃

[ Molecular Weight ]:
376.205

[ Flash Point ]:
238.2±28.7 °C

[ Exact Mass ]:
375.021851

[ PSA ]:
76.50000

[ LogP ]:
4.15

[ Appearance of Characters ]:
white to brown

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.703

[ Storage condition ]:
Store at RT

[ Water Solubility ]:
DMSO: soluble1mg/mL, clear (warmed)

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H315-H319-H335

[ Precautionary Statements ]:
P261-P301 + P310-P305 + P351 + P338

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22-36/37/38

[ Safety Phrases ]:
26

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.